Adult: As conventional tab or solution: Usual dose: 20-30 mg daily in 2-3 divided doses, given 30-45 minutes before meals. Effective dose range: 10-60 mg daily. Max daily dose: 60 mg. Dosage and treatment recommendations may vary among individual products and between countries (refer to specific product guidelines).
Oral Attention deficit hyperactivity disorder
Adult: Individualise dosage based on patient's clinical response and tolerability. As conventional tab or oral solution: Initially, 5 mg once or twice daily; may increase in increments of 5-10 mg in the daily dose at weekly intervals if needed. Max: 100 mg daily in 2-3 divided doses. If effect wears off in the evening causing rebound hyperactivity, an additional dose at bedtime may be appropriate (establish need with trial bedtime dose). As modified-release cap (Medikinet XL or Medikinet MR): For patients new to methylphenidate: Initially, 10 mg daily; may increase in increments of 10 mg in the daily dose at weekly intervals. Daily doses must be given in 2 divided doses (morning and midday). Max daily dose: 1 mg/kg (or 80 mg regardless of body weight). For patients continuing their treatment into adulthood may maintain the same daily dose, provided they experienced clear benefits from the therapy during childhood. As modified-release cap (Ritalin LA or Ritalin XL): For patients not currently taking methylphenidate: Initially, 20 mg once daily; may adjust in increments of 20 mg at weekly intervals. Max daily dose: 80 mg. For patients on methylphenidate: May continue the same daily dose. As modified-release tab (Concerta): For patients not currently taking methylphenidate or who are on stimulants other than methylphenidate: Initially, 18 mg or 36 mg once daily; may increase in increments of 18 mg at weekly intervals. Max daily dose: 72 mg. For patients on methylphenidate: Dosing recommendations should be based on their current dose regimen. Use the lowest effective dose to achieve satisfactory symptom control. Discontinue use if no clinical improvement is achieved after appropriate dose titration within 1 month of treatment. Dosage recommendation is product-specific and may vary based on the chosen brand (refer to specific product guidelines for detailed information). Child: Individualise dosage based on patient's clinical response and tolerability. >6 years As conventional tab or solution: Initially, 5 mg once or twice daily; may increase in increments of 5-10 mg daily at weekly intervals if needed. Max: 60 mg daily in 2-3 divided doses. If effect wears off in the evening causing rebound hyperactivity, an additional dose at bedtime may be appropriate (establish need with trial bedtime dose). As modified-release cap (Medikinet XL or Medikinet MR): Initially, 10 mg daily; may increase at weekly intervals according to response. Max daily dose: 60 mg. As modified-release cap (Ritalin LA or Ritalin XL): Initially, 20 mg once daily. Alternatively, may start at 10 mg once daily if a lower initial dose is appropriate. Dose may be adjusted in increments of 10 mg at weekly intervals. Max daily dose: 60 mg. As modified-release tab (Concerta): Initially, 18 mg once daily; may increase in increments of 18 mg at weekly intervals. Max daily dose: 54 mg. Use the lowest effective dose to achieve satisfactory symptom control. Discontinue use if no clinical improvement is observed after appropriate dose titration within 1 month of treatment. Dosage recommendation is product-specific and may vary based on the chosen brand (refer to specific product guidelines for detailed information).
Child: Individualise dosing titration, final dosage, and wear time based on patient's clinical response and needs. 6-17 years Initially, apply 10 mg (1.1 mg/hour) patch once daily to the hip area 2 hours before an effect is needed and remove 9 hours after application. Dosage may be increased at weekly intervals if needed up to a Max of 3.3 mg/hour. Treatment recommendations may vary among individual products and between countries (refer to specific product guidelines).
What are the brands available for Methylphenidate in Malaysia?
Methylphenidate extended-release prep: May be taken with or without food. Recommendations on taking w/ or w/o food, opening cap, & crushing/chewing are product-specific. Consult product literature for specific instructions. Methylphenidate immediate-release prep: Should be taken on an empty stomach.
Contraindications
Glaucoma, phaeochromocytoma, hyperthyroidism, thyrotoxicosis; diagnosis or history of severe depression, anorexia nervosa or anorexic disorders, psychotic symptoms, severe mood disorders, mania, schizophrenia, psychopathic or borderline personality disorder, suicidal tendencies; diagnosis or history of severe and episodic (type I) bipolar (affective disorder) that is not well controlled; pre-existing CV disorders (including severe hypertension, arterial occlusive disease, angina, haemodynamically significant congenital heart disease, cardiomyopathies, heart failure, MI, potentially life-threatening arrhythmias and channelopathies; known risk factors for or pre-existing cerebrovascular disorders (including cerebral aneurysm), vascular abnormalities (including vasculitis or stroke). Concomitant use or within 14 days of discontinuing MAOIs. Contraindications may vary between individual products and among countries (refer to specific product guidelines).
Special Precautions
Patient with history of seizure disorder; marked anxiety, tension, agitation; diagnosis or family history of Tourette's syndrome or tics; underlying conditions that might be compromised by increased blood pressure or heart rate; known drug or alcohol dependency; emotional instability. Avoid abrupt withdrawal. Not intended for long-term use (>12 months); patients requiring extended therapy must be closely monitored and periodically re-evaluated. Available products or preparations of methylphenidate are not bioequivalent due to pharmacokinetic differences; hence, individual products and certain formulations are not interchangeable on a mg-per-mg basis (refer to specific product guidelines for detailed information). Renal and hepatic impairment. Children. Pregnancy and lactation.
Adverse Reactions
Significant: New-onset or exacerbation of pre-existing psychiatric disorders, psychotic or manic symptoms, aggression or hostility, motor and verbal tics; precipitation of mixed/manic episode (particularly in patients with bipolar disorder); worsening of pre-existing anxiety, agitation or tension; peripheral vasculopathy (including Raynaud's phenomenon); weight loss and growth retardation (particularly in children receiving long-term therapy); angle closure glaucoma, increased IOP, blurred vision; prolonged and painful erections; may decrease seizure threshold resulting in new onset or breakthrough seizure (particularly in patients with history of seizure disorder). Very rarely, cerebral vasculitis. Cardiac disorders: Arrhythmia, palpitations. Gastrointestinal disorders: Abdominal pain, diarrhoea, nausea, stomach discomfort, vomiting, dry mouth. General disorders and administration site conditions: Pyrexia; application site reaction (transdermal). Metabolism and nutrition disorders: Anorexia, decreased appetite. Musculoskeletal and connective tissue disorders: Arthralgia. Nervous system disorders: Headache, dizziness, dyskinesia, psychomotor hyperactivity, somnolence. Psychiatric disorders: Insomnia, nervousness, affect lability, aggression, agitation, anxiety, depression, irritability, abnormal behaviour, bruxism. Respiratory, thoracic and mediastinal disorders: Nasopharyngitis, cough, pharyngolaryngeal pain. Skin and subcutaneous tissue disorders: Alopecia, pruritus, rash, urticaria; contact hypersensitivity (transdermal). Potentially Fatal: CV events (including increased blood pressure, tachycardia, stroke, acute MI, sudden cardiac death); risk for abuse, misuse and addiction (that may lead to overdose).
PO/Transdermal: Z (Associated with small increased risk of cardiac malformations. Consider foetal ECG if methylphenidate is required in first trimester.)
Patient Counseling Information
This drug may cause dizziness, drowsiness or visual disturbances, if affected, do not drive or operate machinery. Avoid exposing the application site of the patch to direct external heat sources (e.g. electric blankets, hair dryers, heating pads).
Monitoring Parameters
Obtain CBC with differential and platelet count periodically (prolonged use). Perform cardiac evaluation at baseline and as clinically indicated. Monitor blood pressure, heart rate, growth rate (height and weight), and appetite. Screen for bipolar disorder and Tourette's syndrome (including family history) before treatment. Assess for signs and symptoms of peripheral vasculopathy, sleep and behavioural changes, worsening of tics or Tourette syndrome; increased IOP (particularly in patients with history of glaucoma); misuse, abuse or substance use disorder; psychotic or manic symptoms; worsening or development of aggressive behaviour or hostility (particularly in children). Transdermal: Assess for signs of worsening erythema, blistering or oedema that spreads beyond the patch site or does not improve within 48 hours of patch removal.
Overdosage
Symptoms: Vomiting, headache, tremor, agitation, muscle twitching, mydriasis, hyperpyrexia, hallucinations, euphoria, confusion, delirium, sweating, flushing, hypertension, dryness of mucous membranes, rhabdomyolysis, tachycardia, palpitations. Management: Symptomatic and supportive treatment. Induce vomiting, followed by administration of activated charcoal if the patient is conscious, or perform gastric lavage with the airway protected for those with depressed respiration, and hyperactive or unconscious patients. In cases of clinically significant hypocalcaemia, the reversal can be achieved through supplementation of oral Ca and/or Ca gluconate infusion.
Drug Interactions
May reduce the effectiveness of antihypertensives. Increased risk of hypertensive crisis with other agents that elevate blood pressure. Enhanced risk of sudden increase in blood pressure and heart rate during surgery when concomitantly given with halogenated anaesthetics. Increased risk of extrapyramidal symptoms with risperidone. Potentially Fatal: Concomitant use or within 14 days of discontinuing MAOIs may increase the risk of hypertensive crisis.
Food Interaction
May exacerbate the CNS adverse effect with alcohol.
Lab Interference
May cause a false-positive result in the urine detection of amphetamines or methamphetamines.
Action
Description: Mechanism of Action: Methylphenidate, a piperidine-derivative CNS stimulant, inhibits the norepinephrine and dopamine reuptake into presynaptic neuron, thereby increasing the release of these neurotransmitters in the extraneuronal space. It also appears to stimulate the cerebral cortex and subcortical structures, leading to increased motor activity. Pharmacokinetics: Absorption: Readily absorbed from the gastrointestinal tract (oral). Increased absorption when applied to inflamed skin or exposed to heat (transdermal). Time to peak plasma concentration: Approx 2 hours (conventional form); approx 8-10 hours (transdermal). Distribution: Enters breast milk. Plasma protein binding: 10-33%. Volume of distribution: 2.65 ± 1.11 L/kg (d-methylphenidate); 1.80 ± 0.91 L/kg (l-methylphenidate). Metabolism: Extensively metabolised mainly via de-esterification by carboxylesterase CES1A1 into α-phenyl-piperidine acetic acid (PPPA; ritalinic acid). Undergoes extensive first-pass metabolism. Excretion: Via urine (78-97% as metabolites and unchanged drug); faeces (1-3%). Elimination half-life: Approx 2 hours (oral); approx 3-4 hours (transdermal).
Chemical Structure
Methylphenidate Source: National Center for Biotechnology Information. PubChem Database. Methylphenidate, CID=4158, https://pubchem.ncbi.nlm.nih.gov/compound/Methylphenidate (accessed on Jan. 22, 2020)
Storage
Oral solution: Store between 20-25°C. Tab/Cap/Transdermal patch: Store between 15-30°C. Protect the tab or cap from light and moisture. Do not refrigerate or freeze the transdermal patch. Storage recommendations may vary between individual products and among countries (refer to specific product guidelines).
N06BA04 - methylphenidate ; Belongs to the class of centrally-acting sympathomimetics. Used as CNS stimulant.
References
Anon. Methylphenidate. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 08/07/2024.Brayfield A, Cadart C (eds). Methylphenidate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 21/11/2024.Concerta Extended-release Tablets (Johnson & Johnson Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 08/07/2024.Concerta Tablet, Extended Release (Janssen Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 21/11/2024.Concerta XL 27 mg Prolonged-release Tablets (Janssen-Cilag Limited). MHRA. https://products.mhra.gov.uk. Accessed 08/07/2024.Daytrana Patch (Noven Therapeutics, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 21/11/2024.Janssen-Cilag (New Zealand) Ltd. Concerta Extended-release Tablets data sheet 3 July 2024. Medsafe. http://www.medsafe.govt.nz. Accessed 21/11/2024.Joint Formulary Committee. Methylphenidate Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 21/11/2024.Medikinet MR 5 mg, 10 mg, 20 mg, 30 mg and 40 mg Hard Capsules (Hyphens Pharma Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 08/07/2024.Medikinet XL 20 mg Modified-release Capsules, Hard (Medice Arzneimittel Putter GmbH & Co. KG). MHRA. https://products.mhra.gov.uk. Accessed 08/07/2024.Methylphenidate Hydrochloride Solution (Ascend Laboratories, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 08/07/2024.Methylphenidate. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 21/11/2024.Novartis New Zealand Limited. Ritalin Tablets and Ritalin LA 10 mg, 20 mg, 30 mg, 40 and 60 mg Capsules data sheet 30 January 2024. Medsafe. http://www.medsafe.govt.nz. Accessed 08/07/2024.Ritalin 10 mg Tablets (InfectoPharm Arzneimittel und Consilium GmbH). MHRA. https://products.mhra.gov.uk. Accessed 08/07/2024.Ritalin and Ritalin LA (Novartis Corporation [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 08/07/2024.Ritalin Capsule, Extended Release (Novartis Pharmaceuticals Corporation). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 21/11/2024.Ritalin Tablet (Novartis Pharmaceuticals Corporation). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 21/11/2024.Ritalin XL 10 mg, 20 mg, 30 mg, 40 mg and 60 mg Modified-release Hard Capsules (InfectoPharm Arzneimittel und Consilium GmbH). MHRA. https://products.mhra.gov.uk. Accessed 08/07/2024.
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